JANSSENS, FRANS EDUARD,严森,嚴森,SCHOENTJES, BRUNO,布鲁诺,布魯諾,COUPA, SOPHIE,柯帕,PONCELET, ALAIN PHILIPPE,彭思特,SIMONNET, YVAN RENE FERDINAND,史孟特
申请号：
TW094110663
公开号：
TWI360548B
申请日:
2005.04.04
申请国别(地区):
TW
年份:
2012
代理人:
摘要：
This invention concerns substituted diaza-spiro-[4.5]-decane derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK2 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incontinence. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.本發明有關經取代二氮雜-螺-[4.5]-癸烷衍生物，其具有神經激肽拮抗活性，尤其是NK1拮抗活性、結合NK1/NK2拮抗活性、結合NK1/NK3拮抗活性及結合NK1/NK2/NK3拮抗活性，其製備、含彼之組成物及其作為藥劑之用途，尤其是用於治療及/或預防精神分裂症，嘔吐，焦慮及抑鬱，應激性大腸徵候群(IBS)，晝夜節律失調，子癇前期，傷害感受，疼痛，尤其是內臟及神經病性疼痛，胰腺炎、神經源性發炎、氣喘、慢性阻塞性肺病(COPD)及排尿障礙，諸如尿失禁。；本發明化合物可由通式(I)表示且亦包括其醫藥上可接受之酸或鹼加成鹽、其立體化學異構形式、其N-氧化物形式及其前藥，其中所有取代基皆如申請專利範圍第1項所定義。
